Human topoisomerase IB is a target of a thiosemicarbazone copper(II) complex.

Authors :: Vutey V
Castelli S
D'Annessa I
Sâmia LB
Souza-Fagundes EM
Beraldo H
Desideri A
Source :: Archives of biochemistry and biophysics [Arch Biochem Biophys] 2016 Sep 15; Vol. 606, pp. 34-40. Date of Electronic Publication: 2016 Jul 16.
Publication Year :: 2016
Abstract: The human topoisomerase IB inhibition and the antiproliferative activity of 3-(4-bromophenyl)-1-pyridin-2-ylprop-2-en-1-one thiosemicarbazone HPyCT4BrPh alone and its copper(II) complex [Cu(PyCT4BrPh)Cl] was investigated. [Cu(PyCT4BrPh)Cl] inhibits both the DNA cleavage and religation step of the enzyme, whilst the ligand alone does not display any effect. In addition we show that coordination to copper(II) improves the cytotoxicity of HPyCT4BrPh against THP-1 leukemia and MCF-7 breast cancer cells. The data indicate that the copper(II) thiosemicarbazone complex may hit human topoisomerase IB and that metal coordination can be useful to improve cytotoxicity of this versatile class of compounds.<br /> (Copyright © 2016 Elsevier Inc. All rights reserved.)